RESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: The study of traditional remedies used by the Chayahuita, an ethnic group from the Peruvian Amazonia, has prompted us to investigate in detail the ethanolic extract of Pseudelephantopus spicatus (Juss. ex Aubl.) C.F. Baker, which has demonstrated strong biological activity towards Leishmania amazonensis. Our goal was to discover the active compound of this plant-based remedy. MATERIALS AND METHODS: A bioguided fractionation of the crude extract was undertaken based on the biological activity recorded against Leishmania amazonensis axenic amastigotes in in vitro bioassays. RESULTS: Three strongly to moderately active compounds were isolated: two hirsutinolides (the 8,13-diacetyl-piptocarphol and the 8-acetyl-13-O-ethyl-piptocarphol) and ursolic acid. IC(50) against Leishmania amazonensis axenic amastigotes are respectively 0.2, 0.37 and 0.99 µM (while IC(50) of amphotericin B is 0.41 µM). These compounds have never been isolated from this plant species, and germacranolides have never been identified as potential antileishmanial agents. CONCLUSIONS: The compounds isolated from Pseudelephantopus spicatus account for the antileishmanial activity of the plant, thus giving support to its use by the Chayahuita in Peru.
Assuntos
Asteraceae , Lactonas/farmacologia , Leishmania/efeitos dos fármacos , Extratos Vegetais/farmacologia , Sesquiterpenos/farmacologia , Tripanossomicidas/farmacologia , Anfotericina B/farmacologia , Asteraceae/química , Fracionamento Químico , Relação Dose-Resposta a Droga , Humanos , Indígenas Sul-Americanos , Concentração Inibidora 50 , Lactonas/química , Lactonas/isolamento & purificação , Leishmania/crescimento & desenvolvimento , Medicina Tradicional , Peru , Componentes Aéreos da Planta , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Plantas Medicinais , Sesquiterpenos/química , Sesquiterpenos/isolamento & purificação , Triterpenos/farmacologia , Tripanossomicidas/química , Tripanossomicidas/isolamento & purificação , Ácido UrsólicoRESUMO
AIM OF THE STUDY: A knowledge attitude and practice study centred on leishmaniasis and its treatment was performed among the Chayahuita, an Amazonian Peruvian ethnic group living in an endemic area. This study documents traditional Chayahuita plant's use and disease concepts. Also, activity of some medicinal plants used by the Chayahuita is highlighted and discussed. MATERIALS AND METHODS: Ninety-three Chayahuita people were interviewed, following a semi-structured questionnaire focussed on disease knowledge and perception, personal attitude and healing practices. Simultaneously, a collection of plants was performed in different ecotopes, in order to make an extensive inventory of the pharmacopoeia. RESULTS: For the Chayahuita, cutaneous (CL) and muco-cutaneous leishmaniasis (MCL) are considered as diseases of their own, with specific names, aetiologies, mode of transmission. Regarding CL, Chayahuita people consider that the humid characteristic of the skin ulcer is a discriminative fact orienting the diagnostic forTa'ta' (leishmaniasis). Forty-six different species were designated useful against LC and /or MCL (29 species by means of the questionnaire and 27 species when collecting in different ecotopes). Thirty-seven extracts corresponding to 31 species used medicinally were screened in vitro against Leishmania amazonensis axenic amastigotes, assessing their viability by the reduction of tetrazolium salt (MTT). Six species displayed a good activity (10 microg/mlAssuntos
Conhecimentos, Atitudes e Prática em Saúde
, Leishmania/efeitos dos fármacos
, Leishmaniose/tratamento farmacológico
, Leishmaniose/etnologia
, Medicina Tradicional
, Humanos
, Testes de Sensibilidade Microbiana/métodos
, Peru/etnologia
, Fitoterapia
, Plantas Medicinais
RESUMO
In the main markets of Paramaribo (Suriname), many stands offer what is locally called "Bitter-cups", or "Kwasi bita beker", small footed-cups, roughly carved from a whitish wood. The use of these cups is strictly medicinal and it seems to be restricted to Suriname, as they are not found in neighbouring countries (Guyana, French Guiana). The aim of this study was to identify the botanical origin of Bitter-cups still in use in the Saramaka traditional medicine (as information from field people was controversial), and document the ethnopharmacology of this original galenical artefact. Microscopic and high performance liquid chromatography (HPLC) analyses were carried out on Bitter-cup, and anatomical criteria (marginal parenchyma band, size of intervessel and vessel-ray pits, rays width and rays composition, vessels clustering, frequency and size of parenchyma pits) together with HPLC profiles of the macerates showed that the wood cup was similar to Quassia amara L. (Simaroubaceae) wood. Ethnopharmacological investigation indicates that the use of these cups is simply due to the pharmacological properties attributed to "bitters", and is strongly linked to tradition and cultural attitudes. This study also emphasizes the long lasting use of these cups, now restricted to Suriname only, with almost no variation over one century.
Assuntos
Etnofarmacologia , Medicina Tradicional , Farmácia/instrumentação , Quassia , Madeira/análise , Cromatografia Líquida de Alta Pressão , História do Século XIX , História do Século XX , Humanos , Teste de Materiais , Medicina Tradicional/história , Microscopia , SurinameRESUMO
In French Guiana, Quassia amara L. (Simaroubaceae) leaf tea is a well-known widely used traditional antimalarial remedy. Impact of the vegetal sampling condition on in vivo and in vitro antimalarial activity was assessed. Traditional infusions were prepared with juvenile or mature leaves, both either fresh or dried. Results showed that growing stage and freshness of vegetal material exert a striking effect on antimalarial activity, both in vitro and in vivo. By far, leaf tea made from fresh juvenile (FJ) Quassia amara leaves was the most active. In vitro, active component (simalikalactone D) concentration correlates biological activities, although unexplained subtle variations were observed. In vivo, tea made with dried juvenile (DJ) leaves displays a peculiar behavior, meaning that some components may help simalikalactone D delivery or may be active in vivo only, therefore enhancing the expected curative effect of the traditional preparation.
Assuntos
Antimaláricos/farmacologia , Bebidas , Dessecação , Malária/tratamento farmacológico , Plasmodium falciparum/efeitos dos fármacos , Plasmodium yoelii , Quassia/crescimento & desenvolvimento , Animais , Antimaláricos/química , Antimaláricos/normas , Antimaláricos/uso terapêutico , Cromatografia Líquida de Alta Pressão , Guiana Francesa , Malária/parasitologia , Camundongos , Testes de Sensibilidade Parasitária , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/crescimento & desenvolvimento , Controle de Qualidade , Quassia/química , Quassinas/análiseRESUMO
French Guiana (North-East Amazonia) records high malaria incidence rates. The traditional antimalarial remedy most widespread there is a simple tea made out from Quassia amara L. leaves (Simaroubaceae). This herbal tea displays an excellent antimalarial activity both in vitro and in vivo. A known quassinoid, simalikalactone D (SkD), was identified as the active compound, with an IC(50) value of 10nM against FcB1 Plasmodium falciparum chloroquine resistant strain in vitro. Lastly, it inhibits 50% of Plasmodium yoelii yoelii rodent malaria parasite at 3.7 mg/kg/day in vivo by oral route. These findings confirm the traditional use of this herbal tea.